Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors

  • Bioorg Med Chem Lett. 2004 Jan 19;14(2):499-504. doi: 10.1016/j.bmcl.2003.10.027.
Sunil K Singh  1 ,  P Ganapati Reddy ,  K Srinivasa Rao ,  Braj B Lohray ,  P Misra ,  Shaikh A Rajjak ,  Yeleswarapu K Rao ,  A Venkateswarlu
Affiliations
  • 1. Discovery Chemistry, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, 500 049, Miyapur, Hyderabad, India. [email protected]
PMID: 14698190 DOI: 10.1016/j.bmcl.2003.10.027
Abstract

Several chemical modifications in the N(1)-benzenesulfonamide ring of celecoxib are presented. The series with a hydroxymethyl group adjacent to the sulfonamide was found to be the most potent modification that yielded many compounds selectively active against COX-2 enzyme in vitro.